Abstract C51: In vitro cytotoxicity of 3-arylcoumarin derivatives in human prostate (PC3) cancer cell line

Abstract

Abstract Coumarins are classified as a member of the benzopyrone family of compounds with diverse and interesting biological activities. They have been used as therapeutic agents in the treatment of various diseases. In the present study, we evaluated the in vitro cytotoxic activity of 3-arylcoumarins (1-11) in human prostate (PC3) cancer and (WPE1-NA22) normal cell lines at various concentrations (0, 10, 25, 50, 75 and 100 μM) after 48 h treatment using crystal violet dye binding assay. The most active compounds cytotoxicity was examined by cell cycle analysis, reactive oxygen species (ROS) production, mitochondrial membrane potential (MMP) measurement and Bax protein expression. Our findings indicate Result that 8-(acetyloxy)-3-(4-methanesulfonylphenyl)-2-oxo-2H-chromen-7-ylacetate (11) showed cytotoxic activity in PC3 cancer cell line (LD50 = 35.0 μM) and no cytotoxic activity in WPE1-NA22 normal cell line (inactive; LD50 = >100 μM) in comparison to the other synthesized analogs. Furthermore, It caused significant cells arrest (p<0.05) in –G1 phase, increase in ROS production, loss of MMP and increase (up-regulation) of Bax protein expression. These findings suggest that these compounds could serve as new leads for the development of novel synthetic compounds with enhanced anticancer activity. Grant Support: Research supported by Florida A & M University Title III Program Citation Format: Musiliyu A. Musa, Moise Y. Joseph, Lekan M. Latinwo, Veera L. Badisa. In vitro cytotoxicity of 3-arylcoumarin derivatives in human prostate (PC3) cancer cell line. [abstract]. In: Proceedings of the Sixth AACR Conference: The Science of Cancer Health Disparities; Dec 6–9, 2013; Atlanta, GA. Philadelphia (PA): AACR; Cancer Epidemiol Biomarkers Prev 2014;23(11 Suppl):Abstract nr C51. doi:10.1158/1538-7755.DISP13-C51